JO3078B1 - Morpholinothiazoles as alpha 7 positive allosteric modulators - Google Patents

Morpholinothiazoles as alpha 7 positive allosteric modulators

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Publication number
JO3078B1
JO3078B1 JOP/2010/0392A JOP20100392A JO3078B1 JO 3078 B1 JO3078 B1 JO 3078B1 JO P20100392 A JOP20100392 A JO P20100392A JO 3078 B1 JO3078 B1 JO 3078B1
Authority
JO
Jordan
Prior art keywords
positive allosteric
allosteric modulators
morpholinothiazoles
alpha
relates
Prior art date
Application number
JOP/2010/0392A
Other languages
Arabic (ar)
Inventor
BOECK Benoît Christian Albert Ghislain DE
Joseph Elisabeth Leenaerts
Gregor James Macdonald
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Application granted granted Critical
Publication of JO3078B1 publication Critical patent/JO3078B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions 10 containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists
JOP/2010/0392A 2009-11-27 2010-11-10 Morpholinothiazoles as alpha 7 positive allosteric modulators JO3078B1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09177347 2009-11-27

Publications (1)

Publication Number Publication Date
JO3078B1 true JO3078B1 (en) 2017-03-15

Family

ID=42010343

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2010/0392A JO3078B1 (en) 2009-11-27 2010-11-10 Morpholinothiazoles as alpha 7 positive allosteric modulators

Country Status (26)

Country Link
US (1) US8637510B2 (en)
EP (1) EP2504333B1 (en)
JP (1) JP5636434B2 (en)
KR (1) KR101749953B1 (en)
CN (1) CN102639530B (en)
AR (1) AR079205A1 (en)
AU (1) AU2010323175B2 (en)
BR (1) BR112012012657A2 (en)
CA (1) CA2780218C (en)
CL (1) CL2012001366A1 (en)
CO (1) CO6531464A2 (en)
DK (1) DK2504333T3 (en)
EA (1) EA020275B1 (en)
ES (1) ES2549917T3 (en)
HK (1) HK1171449A1 (en)
IL (1) IL219926A0 (en)
JO (1) JO3078B1 (en)
MX (1) MX349585B (en)
MY (1) MY160728A (en)
NZ (1) NZ600138A (en)
PL (1) PL2504333T3 (en)
SG (1) SG181054A1 (en)
TW (1) TWI473803B (en)
UA (1) UA106636C2 (en)
WO (1) WO2011064288A1 (en)
ZA (1) ZA201203856B (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10164139A1 (en) 2001-12-27 2003-07-10 Bayer Ag 2-heteroaryl carboxamides
MX2010004177A (en) * 2007-10-18 2010-05-03 Janssen Pharmaceutica Nv Trisubstituted 1,2,4-triazoles.
JO2784B1 (en) * 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 1,3,5-trisubstitued triazole derivative
AR070936A1 (en) * 2008-03-19 2010-05-12 Janssen Pharmaceutica Nv 1,2,4-TRISUSTITUTED TRIAZOLS
AR071763A1 (en) * 2008-05-09 2010-07-14 Janssen Pharmaceutica Nv TRISUSTITUTED PIRAZOLS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND USES OF THE SAME IN THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
BR112012029237A2 (en) 2010-05-17 2016-11-29 Envivo Pharmaceuticals Inc (r) -7-chloro-n- (quinuclidin-3-yl) benzo [b] thiophene-2-carboxamide hydrochloride crystalline form
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
AU2012213086B2 (en) 2011-02-03 2016-05-05 Lupin Limited Pyrrole derivatives used as modulators of alpha7 nAChR
EA024170B1 (en) 2011-02-23 2016-08-31 Люпин Лимитед HETEROARYL DERIVATIVES AS ALPHA7 nAChR MODULATORS
US9187420B2 (en) 2011-03-31 2015-11-17 Lupin Limited Pyrrole derivatives as nicotinic acetylcholine receptor modulators for use in the treatment of neurodegenerative disorders such as alzheimer's and parkinson's disease
WO2013005153A1 (en) 2011-07-05 2013-01-10 Lupin Limited Biaryl derivatives as nachr modulators
IN2014MN01756A (en) * 2012-03-06 2015-07-03 Lupin Ltd
RU2635522C2 (en) 2012-05-08 2017-11-13 Форум Фармасьютикалз, Инк. Methods for cognitive function support, treatment or improvement
EP2945936A1 (en) 2012-11-12 2015-11-25 Lupin Limited Thiazole derivatives as alpha 7 nachr modulators
EP2945941B1 (en) 2013-01-16 2016-12-07 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
WO2014141091A1 (en) 2013-03-13 2014-09-18 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
TW201446243A (en) 2013-06-03 2014-12-16 Lupin Ltd 4-(5-(4-chlorophenyl)-2-(2-cyclopropylacetyl)-1,4-dimethyl-1H-pyrrol-3-yl)benzenesulfonamide as alpha 7 nAChR modulator
CA2913987A1 (en) 2013-06-17 2014-12-24 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
AU2017313390A1 (en) * 2016-08-19 2019-03-07 The University Of Bristol Cytisine derivatives for the treatment of addiction
US20220040158A1 (en) * 2018-09-24 2022-02-10 Astrazeneca Ab Azd0328 dosage regime for treating cognitive impairment
US20220347166A1 (en) * 2019-10-21 2022-11-03 Cambridge Cognition Limited Schizophrenic Disorder Treatment using Combination Therapy
CN115317480B (en) * 2022-09-01 2023-05-16 新乡医学院 Pharmaceutical use of N- (3-methyl-5-isothiazolyl) -2-oxo-3- (2H) -benzoxazole acetamide

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004506735A (en) * 2000-08-18 2004-03-04 ファルマシア・アンド・アップジョン・カンパニー Quinuclidine-substituted aryl compounds for disease treatment
US8178570B2 (en) 2003-04-09 2012-05-15 Exelixis, Inc. Tie-2 modulators and methods of use
EP1884513A4 (en) 2005-05-23 2010-04-28 Japan Tobacco Inc Pyrazole compound and therapeutic agent for diabetes comprising the same
EP1926719B1 (en) * 2005-09-13 2017-05-31 Janssen Pharmaceutica NV 2-aniline-4-aryl substituted thiazole derivatives
CN101374810A (en) * 2006-01-18 2009-02-25 锡耶纳生物技术股份公司 Modulators of alpha7 nicotinic acetylcholine receptors and therapeutic uses thereof
JO3019B1 (en) * 2006-04-19 2016-09-05 Janssen Pharmaceutica Nv Trisubstituted 1,2,4-Triazoles
KR20100133016A (en) * 2008-04-17 2010-12-20 글락소 그룹 리미티드 Indoles as modulators of nicotinic acetylcholin receptor subtype alpha-71
JP2016536338A (en) 2013-09-09 2016-11-24 メリンタ セラピューティクス，インコーポレイテッド Antimicrobial compounds and methods for their production and use

Also Published As

Publication number Publication date
NZ600138A (en) 2013-05-31
CO6531464A2 (en) 2012-09-28
KR20120102083A (en) 2012-09-17
EA201290394A1 (en) 2012-10-30
CL2012001366A1 (en) 2012-10-05
CN102639530A (en) 2012-08-15
EP2504333A1 (en) 2012-10-03
JP5636434B2 (en) 2014-12-03
CA2780218A1 (en) 2011-06-03
AU2010323175B2 (en) 2014-06-26
IL219926A0 (en) 2012-07-31
DK2504333T3 (en) 2015-10-19
MX349585B (en) 2017-08-03
WO2011064288A1 (en) 2011-06-03
TW201127836A (en) 2011-08-16
AU2010323175A1 (en) 2012-05-10
AR079205A1 (en) 2012-01-04
UA106636C2 (en) 2014-09-25
MX2012006082A (en) 2012-06-19
BR112012012657A2 (en) 2016-07-12
CN102639530B (en) 2014-08-06
KR101749953B1 (en) 2017-06-22
TWI473803B (en) 2015-02-21
EP2504333B1 (en) 2015-07-15
ZA201203856B (en) 2015-01-28
US8637510B2 (en) 2014-01-28
US20120238561A1 (en) 2012-09-20
PL2504333T3 (en) 2015-12-31
SG181054A1 (en) 2012-07-30
HK1171449A1 (en) 2013-03-28
JP2013512218A (en) 2013-04-11
EA020275B1 (en) 2014-09-30
ES2549917T3 (en) 2015-11-03
CA2780218C (en) 2018-10-16
MY160728A (en) 2017-03-15

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